Tablet formulation for CGRP active compounds

Abstract

The present invention is directed to compositions comprising an extrudate or solid solution of a compound, or a salt thereof, of Formula I (API): wherein “R a ” is independently —H or —F, in a water-soluble polymer matrix which further comprises a disintegration system allowing a tablet made therefrom to rapidly disintegrate in the environment in which the API is to be released.

The invention claimed is: 
     
       1. A tablet comprising:
 an extrudate comprising:
 a water-soluble polymer matrix; 
 a dispersing agent; and 
 a compound of Formula Ia, or a pharmaceutically acceptable salt thereof: 
 
 
       
         
           
           
               
               
           
         
         
           wherein each of R b  is —H, 
           wherein the compound of Formula Ia is dispersed within the polymer matrix; and 
         
         a disintegration system. 
       
     
     
       2. The tablet according to  claim 1 , wherein the water-soluble polymer matrix is a water-soluble polyvinylpyrrolidone/vinyl acetate (PVP-VA) copolymer. 
     
     
       3. The tablet according to  claim 1 , wherein the disintegration system comprises a disintegrant selected from the group consisting of croscarmellose sodium and crospovidone. 
     
     
       4. The tablet according to  claim 3 , wherein the disintegrant is croscarmellose sodium. 
     
     
       5. The tablet according to  claim 1 , wherein the dispersing agent is selected from the group consisting of d-alpha tocopherol polyethyleneglycol succinate (TPGS) and polyethoxylated castor oil. 
     
     
       6. The tablet according to  claim 5 , wherein the dispersing agent is d-alpha tocopherol polyethyleneglycol succinate (TPGS). 
     
     
       7. The tablet according to  claim 1 , wherein the compound of Formula Ia is present in an amount from about 20 wt % to about 22 wt % of the extrudate. 
     
     
       8. The tablet according to  claim 7 , wherein the extrudate comprises about 50 wt % of the tablet. 
     
     
       9. The tablet according to  claim 1 , wherein the tablet has a hardness of from about 12 kP to about 18 kP. 
     
     
       10. The tablet of  claim 1 , wherein the disintegration system comprises powdered sodium chloride.